GSK-3685032 - 10mM in DMSO , CAS No.2170137-61-6

CAS: 2170137-61-6 Cat. No.: G656729 分子式: C₂₂H₂₄N₆OS 分子量: 420.53

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1 -selective inhibitor, with an IC 50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition

In Vitro

GSK-3685032 (6 days) has cell growth inhibition of majority cancer cell lines, with a median growth IC 50 value of 0.64 μM. GSK-3685032 (0.1-1000 nM, 1-6 days) exhibits growth inhibition after 3 days, with decreasing growth IC 50 throughout a 6 d time course. GSK3685032 (10-10000 nM, day 4) dose-dependently increases the immune-related gene transcription. GSK3685032 (3.2-10,000 nM, 2 days) inhibits DNMT1 protein expression. GSK3685032 induces DNA hypomethylation and gene activation. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: 15 leukemia, 29 lymphoma and 7 multiple myeloma cell lines, e.g., EOL-1, Ki-JK, MM.IR cells. Concentration: 0.01-100 μM Incubation Time: 6 days Result: Showed cell growth inhibition of majority cancer cell lines, with a median growth IC 50 value of 0.64 μM. Cell Proliferation AssayCell Line: MV4-11 cells Concentration: 0.1-1000 nM Incubation Time: 1-6 days Result: Exhibited growth inhibition after 3 days, with decreasing growth IC 50 throughout a 6 d time course. RT-PCRCell Line: MV4-11 cells Concentration: 10-10000 nM Incubation Time: 4 days Result: Dose-dependent increased of CXCL11, IFI27, HLA-DQA1 and MAGEA4 following treatment of MV4-11 cells. Western Blot AnalysisCell Line: GDM-1 cells Concentration: 3.2-10,000 nM Incubation Time: 2 days Result: Inhibited DNMT1 protein expression

In Vivo

GSK-3685032 (1-45 mg/kg; subcutaneous twice daily for 28 days) inhibits tumor growth in the subcutaneous MV4-11 or SKM-1 xenograft models . Summary of mouse pharmacokinetic parameters for GSK-3685032 Dose,Route C max (ng/mL) AUC 0-8hr (h*ng/mL) DNAUC (h*kg*ng/mL/mg) Clearance (mL/min/kg) Volume dss (L/kg) T 1/2 (h) 2 mg/kg,IV 5103 2418 1209 13 1.3 1.8 2 mg/kg,SC 252 921 461 NA NA 2.8 2 mg/kg,SC 5473 15400 513 NA NA ND MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: MV4-11 xenograft models (female CD1-Foxn1 mice, 12 weeks of age) or SKM-1 xenograft models (NOD. CB17-Prkdc 1NCrCrl mice, 8-11 weeks of age) Dosage: 1, 5, 15, 30, 45 mg/kg (10% captisol adjusted to pH 4.5-5 with 1 M acetic acid, stored for up to 1 week at 4 °C) Administration: Subcutaneous injection, twice daily for 4 weeks Result: Revealed statistically significant dose-dependent tumor growth inhibition with clear regression at ≥30 mg/kg.

IC50& Target:DNMT1

Specifications

仕様と純度

10mM in DMSO

生化学的・生理学的メカニズム

GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1 -selective inhibitor, with an IC 50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition.

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

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アクションタイプ

INHIBITOR

名前と識別子

• 分子量: 420.53

よくある質問

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2170137-61-6, the molecular formula is C22H24N6OS, and the molecular weight is 420.53 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.